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Assay Detail

CHEMBL4727484

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at TLR7 in mouse splenocytes assessed as inhibition of ssRNA40-induced IL6 production
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Splenocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Toll-like receptor 7 (CHEMBL6085)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Alper PB,Deane J,Betschart C,Buffet D,Collignon Zipfel G,Gordon P,Hampton J,Hawtin S,Ibanez M,Jiang T,Junt T,Knoepfel T,Liu B,Maginnis J,McKeever U,Michellys PY,Mutnick D,Nayak B,Niwa S,Richmond W,Rush JS,Syka P,Zhang Y,Zhu X
Bioorg Med Chem Lett (2020) 30 : 127366 -127366
PubMed 32738975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.89 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634860 1 8.40
CHEMBL4748638 1 7.42
CHEMBL4740968 1 7.26
CHEMBL4792072 1 7.03
CHEMBL4755173 1 7.01
CHEMBL4783510 1 6.96
CHEMBL4796453 1 6.92
CHEMBL4782200 1 6.82
CHEMBL4776103 1 6.66
CHEMBL4740820 1 6.52
CHEMBL4745239 1 5.92
CHEMBL4743698 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634860 IC50 = 4.0 nM 8.40
CHEMBL4748638 IC50 = 38.0 nM 7.42
CHEMBL4740968 IC50 = 55.0 nM 7.26
CHEMBL4792072 IC50 = 93.0 nM 7.03
CHEMBL4755173 IC50 = 97.0 nM 7.01
CHEMBL4783510 IC50 = 110.0 nM 6.96
CHEMBL4796453 IC50 = 120.0 nM 6.92
CHEMBL4782200 IC50 = 150.0 nM 6.82
CHEMBL4776103 IC50 = 220.0 nM 6.66
CHEMBL4740820 IC50 = 300.0 nM 6.52
CHEMBL4745239 IC50 = 1200.0 nM 5.92
CHEMBL4743698 IC50 = 2000.0 nM 5.70